Pyrimidine hydrazones as potent anticonvulsant
Journal name: World Journal of Pharmaceutical Research
Original article title: Pyrimidine hydrazones as potent anticonvulsant
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Srivastav Sanchit, Shukla Chhama, Luhach Kanishk, Pandeya S. N.
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World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Pyrimidine hydrazones as potent anticonvulsant
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20166-6448
Copyright (license): WJPR: All rights reserved
Summary of article contents:
Introduction
The study presented in the World Journal of Pharmaceutical Research focuses on the synthesis and evaluation of pyrimidine hydrazones as potential anticonvulsant agents. Pyrimidines are well-known heterocyclic compounds recognized for their diverse biological activities, including anticancer and antimicrobial effects. The research explores the formation of hydrazones through the reaction of hydrazine with various ketones and aldehydes, identifying their structural significance in drug development. Schiff bases derived from pyrimidine hydrazones were synthesized and tested for anticonvulsant activity using specific models in mice.
Synthesis of Pyrimidine Hydrazone Derivatives
The synthesis of pyrimidine hydrazone derivatives involved a multi-step process. Initially, ethyl 6-methyl-2-oxo-4-aryl-1,2,3,4-tetrahydro pyrimidin-5-carboxylates were produced through the refluxing of urea, ethylacetoacetate, and aromatic aldehydes in ethanol. Following this, the hydrazone derivatives were synthesized by adding hydrazine hydrate to the previously obtained pyrimidine compounds under acidic conditions. Finally, the resulting compounds were reacted with terpenes such as camphor and citral to form Schiff bases, allowing for the creation of various derivatives of pyrimidine hydrazones that were subsequently evaluated for biological activity.
Anticonvulsant Activity Evaluation
The anticonvulsant activity of the synthesized compounds was assessed using two different models: the Isoniazid induced model and the Thiosemicarbazide model, on male albino mice. Each compound was administered at a dose of 30 mg/kg, and their effects were compared to a standard drug, diazepam. The results indicated that specific compounds, notably SBP-1a and SBP-3c, exhibited significant anticonvulsant properties, demonstrating the potential effectiveness of pyrimidine hydrazone derivatives in managing epilepsy-related conditions.
Neurotoxicity Screening
In addition to evaluating anticonvulsant effects, the research also included a neurotoxicity assessment using the Rota rod test. This test monitored the motor coordination of the mice by determining their ability to remain balanced on a rotating rod. The results showed that none of the synthesized compounds induced neurotoxicity at a dose of 20 mg/kg, suggesting that the tested substances did not adversely affect motor skills. This finding is essential, as it implies that the promising anticonvulsant agents could be administered without causing neurological impairment.
Conclusion
The study successfully synthesized and evaluated pyrimidine hydrazones for their potential as anticonvulsant medications, demonstrating robust pharmacological activity with a favorable safety profile. The synthetic methodology allowed for the creation of various derivatives, leading to the identification of the most active compounds. Through thorough evaluation of both anticonvulsant properties and neurotoxicity, the findings indicate that pyrimidine hydrazones could be valuable candidates for further research and development in anticonvulsant therapy. The research highlights the importance of exploring new chemical entities in drug discovery to address the challenges of existing anticonvulsant medications.
FAQ section (important questions/answers):
What are pyrimidine hydrazones and their significance in drug discovery?
Pyrimidine hydrazones are derivatives of pyrimidine and are known for their various biological activities, including anticonvulsant properties. They play a key role in drug discovery due to their potential effectiveness against diseases.
How are pyrimidine hydrazones synthesized in the study?
Pyrimidine hydrazones are synthesized through a three-step process involving reactions of pyrimidine derivatives with hydrazine, followed by reactions with terpenes like camphor, citral, and menthone to form Schiff bases.
What methods were used to evaluate the anticonvulsant activity?
Anticonvulsant activity was evaluated using Isoniazid and Thiosemicarbazide induced convulsion models on male albino mice, comparing results to a standard drug, diazepam.
What were the results of the anticonvulsant activity evaluation?
The compounds SBP-1a and SBP-3c showed the highest anticonvulsant activity among the screened pyrimidine hydrazones when tested at a dose of 30mg/kg body weight.
How was neurotoxicity assessed in the synthesized compounds?
Neurotoxicity was assessed using the Rotarod test, measuring motor coordination impairment. None of the tested compounds exhibited neurotoxicity at a dose of 20mg/kg.
What is the significance of the findings in this study?
The findings suggest that synthesized pyrimidine hydrazones could be developed for anticonvulsant therapies while demonstrating low neurotoxicity, highlighting their potential for further research in drug development.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Pyrimidine hydrazones as potent anticonvulsant”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Activity:
Activity refers to the effects and actions of synthesized compounds, particularly in the context of their anticonvulsant properties. The research evaluates how these compounds interact within biological systems, measuring their efficacy in preventing seizures induced by specific chemical agents, thus determining their potential therapeutic applications.
2) Camphor:
Camphor is a terpene used in the synthesis of Schiff bases for pyrimidine hydrazone derivatives. In pharmaceutical formulations, camphor exhibits various biological activities, including anti-inflammatory and analgesic effects, making it a valuable component for enhancing the effectiveness of synthesized anticonvulsant agents in research.
3) Drug:
A drug is a chemical substance used for the diagnosis, treatment, or prevention of diseases. In this study, new drug candidates derived from pyrimidine hydrazones were evaluated for their anticonvulsant activity. The research aims to identify potential therapeutic agents that can effectively manage seizure disorders.
4) Table:
Table represents a structured collection of data displaying the results of the synthesized compounds' evaluations. In the context of this research, tables summarize the pharmacological effects, yields, melting points, and other physicochemical properties of the pyrimidine hydrazone derivatives, facilitating comparisons and analyses.
5) Animal:
Animal refers to the living subjects used in scientific experiments, particularly in pharmacological studies. Male albino mice were utilized in this research to assess the anticonvulsant effects of synthesized compounds, allowing researchers to observe biological responses and efficacy in a controlled environment before potential human trials.
6) Male:
Male indicates the sex of the experimental animals used in the study, specifically male albino mice. The choice of male subjects can influence physiological responses and ensure consistent results during pharmacological evaluations, as sex differences may impact drug metabolism and efficacy in anticonvulsant activity.
7) Discussion:
Discussion entails the interpretation and analysis of results obtained from the experiment. In scientific papers, this section reviews the significance of findings, compares them to existing literature, and offers insights into the implications of synthesized compounds in anticonvulsant therapy, addressing potential future research directions.
8) Water:
Water is a solvent used during the synthesis process of organic compounds, including pyrimidine hydrazones. The solubility of certain starting materials and intermediates in water is crucial for effective chemical reactions, ensuring proper mixing and interaction between compounds to achieve successful yields in drug synthesis.
9) Death:
Death signifies the endpoint of physiological processes and is a critical observation in toxicological studies. In this research, the occurrence of death among mice after exposure to synthesized compounds indicates the neurotoxic potential or lethality of certain agents, guiding researchers in determining safety profiles for new drugs.
10) Pharmacological:
Pharmacological pertains to the study of drugs, their mechanisms, effects, and interactions within biological systems. The research focuses on assessing the pharmacological activity of pyrimidine hydrazones, particularly their anticonvulsant properties, which are critical for understanding their potential therapeutic applications in medicine.
11) Lucknow:
Lucknow is the location of one of the institutions involved in the study. The geographical context often reflects the collaboration between academic and research institutions, contributing to the overall research efforts and scientific advancements in the field of pharmaceutical sciences and drug discovery.
12) Shukla (Sukla):
Shukla refers to one of the co-authors of the research and indicates collaboration among multiple researchers in the study. The contributions of each author are essential for comprehensive research outcomes, providing various expertise that enhances the overall quality and depth of the investigation.
13) Feat:
Feat denotes an achievement or accomplishment, particularly in the context of scientific synthesis and compound development. It highlights the successful creation of new pyrimidine hydrazone derivatives with potential anticonvulsant activity, showcasing the innovative efforts of researchers in advancing drug discovery and pharmaceutical development.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Pyrimidine hydrazones as potent anticonvulsant’. Further sources in the context of Science might help you critically compare this page with similair documents:
Anticonvulsant activity, Standard drug, Rotarod test, Schiff Base, Pyrimidine derivatives, Chemical Induced Models, Clonic Seizures, Tonic Seizures, Pharmacological assay.